Carcinostatic composition containing 3-N-o-toluyl-5-fluorouracil producing the same

Abstract

Carcinostatic composition containing an oily substance such as a glyceride and 3-N-o-toluyl-5-fluorouracil suspended therein. The composition exhibits a remarkable carcinostatic effect against various cancerous cells at a low dose and has less side-effects than 5-fluorouracil and its known derivatives which have been typical carcinostatic compounds. A process of producing carcinostatic composition comprises dispersing 1,3-di-N-acyl-5-fluorouracil into an oily substance such as a glyceride to prepare an emulsion and selectively substituting a hydrogen atom only for the 1-position acyl group, whereby the compound is acylated only at the 3-position and which is a chief constituent of the carcionstatic composition.

What is claimed is: 
     
       1. A process for producing a composition containing 3-N-o-toluyl-5-FU which comprises the steps of: (a) dispersing 1,3-di-N-o-toluyl-5-FU in a glyceride selected from the group consisting of triolein, tripalmitin, stearodiolen and palmitooleostearin,   (b) forming an emulsion containing water and a phospholipid,   (c) adding the mixture of (a) to the emulsion of (b) to form a resulting emulsion,   (d) permitting the resulting emulsion to stand at temperatures sufficient to liberate the toluyl group at the 1-position such that substantially all of the 1,3-di-N-o-toluyl-5-FU is converted to 3-N-o-toluyl-5-FU, and   (e) removing the liberated toluyl group from the resulting emulsion.   
     
     
       2. The process according to claim 1 wherein the phospholipid is selected from the group consisting of lecithin and phosphatidic acid. 
     
     
       3. The emulsion produced according to steps (a)-(e) of claim 1.